专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06458843B1 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 有权
标题翻译：碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途
公开(公告)号：US06458843B1
公开(公告)日：2002-10-01
申请号：US09421403
申请日：1999-10-21
申请人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
发明人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
IPC分类号： A61K3117
CPC分类号： C07D213/643 , A61K31/17 , A61K31/175 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , C07C281/12 , C07C281/14 , C07C2601/14 , C07D209/14 , C07D211/46 , C07D213/68 , C07D215/12 , C07D307/91 , C07D309/12 , C07D317/50 , C07D317/58 , C07D317/62 , C07D317/64 , C07D319/18
摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
摘要翻译：本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

2. 发明授权

US06613803B1 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
公开(公告)号：US06613803B1
公开(公告)日：2003-09-02
申请号：US09421403
申请日：1999-10-21
申请人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
发明人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin , Eckard Weber
IPC分类号： A61K3117
CPC分类号： C07D213/643 , A61K31/17 , A61K31/175 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , C07C281/12 , C07C281/14 , C07C2601/14 , C07D209/14 , C07D211/46 , C07D213/68 , C07D215/12 , C07D307/91 , C07D309/12 , C07D317/50 , C07D317/58 , C07D317/62 , C07D317/64 , C07D319/18
摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

3. 发明授权

US06696442B2 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
标题翻译：碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途
公开(公告)号：US06696442B2
公开(公告)日：2004-02-24
申请号：US10178477
申请日：2002-06-25
申请人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin
发明人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin
IPC分类号： A61K3117
CPC分类号： C07D213/643 , A61K31/17 , A61K31/175 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , C07C281/12 , C07C281/14 , C07C2601/14 , C07D209/14 , C07D211/46 , C07D213/68 , C07D215/12 , C07D307/91 , C07D309/12 , C07D317/50 , C07D317/58 , C07D317/62 , C07D317/64 , C07D319/18
摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl-82-; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
摘要翻译：本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基-82-。或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

4. 发明授权

US6124317A 2-substituted piperidine analogs and their use as subtype-selective NMDA receptor antagonists 失效
标题翻译： 2-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US6124317A
公开(公告)日：2000-09-26
申请号：US91593
申请日：1998-11-18
申请人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
发明人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
IPC分类号： A61K31/445 , A61K31/454 , C07D211/14 , C07D401/12 , A01N43/40
CPC分类号： C07D401/12 , A61K31/445 , A61K31/454 , C07D211/14
摘要： Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartatc (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, amioglycoside antibiotics-induced hearing loss, migraine headaches, chronic pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译： PCT No.PCT / US96 / 20767 Sec。 371日期：1998年11月18日 102（e）1998年11月18日日期PCT 1996年12月20日PCT公布。出版物WO97 / 23215 PCT 日期1997年7月3日新颖的2-取代的哌啶类似物，含有它们的药物组合物和使用2-取代的哌啶类似物作为N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂的方法，用于治疗诸如中风脑缺血，中枢神经系统创伤，低血糖，焦虑症，惊厥，阿糖苷类抗生素诱发的听力损失，偏头痛，慢性疼痛，青光眼，CMV视网膜炎，精神病，尿失禁，阿片样物质耐受或戒断，或神经退行性疾病，阿尔茨海默病，帕金森综合征和亨廷顿氏病。

5. 发明授权

US06534525B1 2-substituted piperidine analogs and their use as subtype-selective NMDA receptor antagonists 失效
标题翻译： 2-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US06534525B1
公开(公告)日：2003-03-18
申请号：US09598162
申请日：2000-06-21
申请人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
发明人： Christopher F. Bigge , John F. W. Keana , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Anthony P. Guzikowski
IPC分类号： A61K31445
CPC分类号： C07D401/12 , A61K31/445 , A61K31/454 , C07D211/14
摘要： Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonist of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, chronics pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译：新的2-取代的哌啶类似物，含有它们的药物组合物和使用2-取代的哌啶类似物作为N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂的方法，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，焦虑症，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，脊髓痛，青光眼，CMV视网膜炎，精神病，尿失禁，阿片样物质耐受或戒断，或神经退行性疾病，如幻影，阿尔茨海默病，帕金森综合征并描述亨廷顿氏病。

6. 发明授权

US06124323A 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists 失效
标题翻译： 4-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US06124323A
公开(公告)日：2000-09-26
申请号：US091598
申请日：1998-09-16
申请人： Christopher F. Bigge , Po-Wai Yuen , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana , Anthony P. Guzikowski
发明人： Christopher F. Bigge , Po-Wai Yuen , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana , Anthony P. Guzikowski
IPC分类号： C07D211/14 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/30 , C07D211/38 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04 , A01N43/40 , C07D211/20 , C07D211/26 , C07D211/60
CPC分类号： C07D401/04 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/30 , C07D211/38 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/64 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
摘要翻译： PCT No.PCT / US96 / 20872 Sec。 371日期：1998年9月16日 102（e）1998年9月16日PCT PCT 1996年12月20日PCT公布。第WO97 / 23216号公报日期1997年7月3日新颖的4-取代的哌啶类似物，含有它们的药物组合物和使用4-取代的哌啶类似物的方法是N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，精神病，焦虑症，偏头痛，青光眼，CMV视网膜炎，氨基糖苷类抗生素诱发的听力损失，惊厥，慢性疼痛，阿片样物质耐受或戒断，尿失禁或神经退行性疾病，如幻影，描述了阿尔茨海默病，帕金森综合征和亨廷顿氏病。

7. 发明授权

US6130234A 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists 失效
标题翻译： 4-取代的哌啶类似物及其作为亚型选择性NMDA受体拮抗剂的用途
公开(公告)号：US6130234A
公开(公告)日：2000-10-10
申请号：US91594
申请日：1996-12-20
申请人： Christopher F. Bigge , Jonathan Wright , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
发明人： Christopher F. Bigge , Jonathan Wright , Sui Xiong Cai , Eckard Weber , Richard Woodward , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
IPC分类号： A61K31/00 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/498 , A61K31/505 , A61K31/517 , A61K31/529 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/00 , A61P25/02 , A61P25/04 , A61P43/00 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/54 , C07D211/58 , C07D211/70 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12 , C07D235/08
CPC分类号： C07D401/06 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/54 , C07D211/58 , C07D405/06
摘要： Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.
摘要翻译： PCT No.PCT / US96 / 20766 Sec。 371日期：1998年9月16日 102（e）1998年9月16日PCT PCT 1996年12月20日PCT公布。公开号WO97 / 23214 PCT 日期1997年7月3日新颖的4-取代的哌啶类似物，含有它们的药物组合物和使用4-取代的哌啶类似物作为N-甲基-D-天冬氨酸（NMDA）受体亚型的选择性活性拮抗剂的方法，用于治疗诸如中风，脑缺血，中枢神经系统创伤，低血糖症，焦虑症，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，青光眼，CMV视网膜炎，慢性疼痛，阿片样物质耐受或戒断，或神经退行性疾病，如幻影，阿尔茨海默病，帕金森综合征并描述亨廷顿氏病。还描述了制备4-取代的哌啶类似物和4-取代的哌啶类似物的新中间体的新方法。

8. 发明授权

US06680332B1 Substituted 5-oxo-5,6,7,8-tetrahydro-4H-1-benzopyrans and benzothiopyrans and the use thereof as potentiators of AMPA 失效
标题翻译：取代的5-氧代-5,6,7,8-四氢-4H-1-苯并吡喃和苯并噻喃并将其作为AMPA的增效剂
公开(公告)号：US06680332B1
公开(公告)日：2004-01-20
申请号：US09980628
申请日：2002-05-20
申请人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
发明人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
IPC分类号： A61K4364
CPC分类号： C07D311/74
摘要： Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.
摘要翻译：本发明公开了一种治疗患有AMPA受体AMPA受体阳性调节的病症的方法，其包括向有需要的动物施用式I化合物或其药学上可接受的盐或前药，其中：Y为NH 2， NHR和NHCOR; Z是O和S; 并且R1，R2，R3，R4和X在本文中定义。这些化合物可用作认知增强剂，用于治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿舞蹈病，帕金森病，AIDS相关性痴呆和唐氏综合征，以及治疗精神分裂症和肌阵挛。还公开了可用于治疗对AMPA受体的正调节起反应的病症的药物组合物和式I的新化合物。

9. 发明授权

US06800657B2 Substituted 5-oxo-5, 6, 7, 8-tetrahydro-4H-1-benzopyrans 失效
标题翻译：取代的5-氧代-5,6,7,8-四氢-4H-1-苯并吡喃
公开(公告)号：US06800657B2
公开(公告)日：2004-10-05
申请号：US10610871
申请日：2003-07-02
申请人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
发明人： Christopher S. Konkoy , David B. Fick , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana
IPC分类号： A61K3138
CPC分类号： C07D311/74
摘要： Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.
摘要翻译：本发明公开了一种治疗患有AMPA受体AMPA受体阳性调节的病症的方法，其包括向有需要的动物施用式I化合物或其药学上可接受的盐或前药，其中：Y为NH 2， NHR和NHCOR; Z是O和S; 并且R1，R2，R3，R4和X在本文中定义。这些化合物可用作认知增强剂，用于治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿舞蹈病，帕金森病，AIDS相关性痴呆和唐氏综合症，以及治疗精神分裂症和肌阵挛。还公开了可用于治疗对AMPA受体的正调节起反应的病症的药物组合物和式I的新化合物。

10. 发明授权

US06534522B2 Subtype-selective NMDA receptor ligands and the use thereof 失效
标题翻译：亚型选择性NMDA受体配体及其用途
公开(公告)号：US06534522B2
公开(公告)日：2003-03-18
申请号：US09779024
申请日：2001-02-07
申请人： Christopher F. Bigge , Gian Luca Araldi , Sui Xiong Cai , Anthony P. Guzikowski , Donald Lamunyon , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
发明人： Christopher F. Bigge , Gian Luca Araldi , Sui Xiong Cai , Anthony P. Guzikowski , Donald Lamunyon , Nancy C. Lan , Zhang-Lin Zhou , John F. W. Keana
IPC分类号： C07D40112
CPC分类号： C07D239/06 , C07D211/14 , C07D211/18 , C07D217/04 , C07D221/16 , C07D221/28 , C07D233/26 , C07D451/06 , C07D471/04
摘要： The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
摘要翻译：本发明涉及亚型选择性NMDA受体配体及其用于治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失的用途，以及治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征，治疗或预防兴奋性氨基酸过度刺激的不良后果，治疗焦虑症，精神病，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，慢性疼痛，帕金森病，青光眼，CMV视网膜炎，尿失禁，阿片样物质容忍或戒断，诱导麻醉以及增强认知。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式